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WO2002062778A3 - Antithrombotische verbindungen, deren herstellung und deren verwendung als arzneimittel - Google Patents

Antithrombotische verbindungen, deren herstellung und deren verwendung als arzneimittel Download PDF

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Publication number
WO2002062778A3
WO2002062778A3 PCT/EP2002/000823 EP0200823W WO02062778A3 WO 2002062778 A3 WO2002062778 A3 WO 2002062778A3 EP 0200823 W EP0200823 W EP 0200823W WO 02062778 A3 WO02062778 A3 WO 02062778A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
general formula
worthwhile
thrombotic
group substituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2002/000823
Other languages
English (en)
French (fr)
Other versions
WO2002062778A2 (de
Inventor
Uwe Joerg Ries
Henning Priepke
Herbert Nar
Jean-Marie Stassen
Wolfgang Wienen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals Inc
Original Assignee
Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from DE10104597A external-priority patent/DE10104597A1/de
Application filed by Boehringer Ingelheim Pharma GmbH and Co KG, Boehringer Ingelheim Pharmaceuticals Inc filed Critical Boehringer Ingelheim Pharma GmbH and Co KG
Priority to EP02714118A priority Critical patent/EP1390357A2/de
Priority to CA002435492A priority patent/CA2435492A1/en
Priority to JP2002563132A priority patent/JP2004522759A/ja
Priority to MXPA03006648A priority patent/MXPA03006648A/es
Publication of WO2002062778A2 publication Critical patent/WO2002062778A2/de
Anticipated expiration legal-status Critical
Publication of WO2002062778A3 publication Critical patent/WO2002062778A3/de
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Die vorliegende Erfindung betrifft antithrombotische Verbindungender allgemeinen Formel (1), in der R1 bis R4, Ar, A, m und n wie im Anspruch 1 definiert sind, deren Tautomere, deren Stereoisomere, deren Gemische, deren Prodrugs und deren Salze, welche wertvolle Eigenschaften aufweisen. Die Verbindungen der obigen allgemeinen Formel 1, in denen Ar eine durch die Reste R5, R6 und R7 substituierte Phenyl-oder Naphthylgruppe und R5 eine Cyanogruppe darstellt, stellen wertvolle Zwischenprodukte zur Herstellung der entsprechenden Verbindungen der allgemeinen Formel 1 dar, in denen R5 eine gegebenenfalls durch eine oder zwei C1-3-Alkylgruppen substituierte Amidinogruppe bedeutet. Die Vergindungen der obigen allgemeinen Formel 1 mit Ausnahme derjenigen Vergindungen, in denen Ar eine durch die Reste R5, R6 und R7 substituierte Phenyl- oder Naphthylgruppe und R5 eine Cyanogruppe darstellt, weisen wertvolle pharmakologische Eigenschaften auf, insbesondere eine antithrombotische Wirkung und eine Faktor Xainhibierende Wirkung.
PCT/EP2002/000823 2001-02-02 2002-01-26 Antithrombotische verbindungen, deren herstellung und deren verwendung als arzneimittel Ceased WO2002062778A2 (de)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP02714118A EP1390357A2 (de) 2001-02-02 2002-01-26 Antithrombotische verbindungen, deren herstellung und deren verwendung als arzneimittel
CA002435492A CA2435492A1 (en) 2001-02-02 2002-01-26 Antithrombotic compounds, the preparation thereof and their use as pharmaceutical compositions
JP2002563132A JP2004522759A (ja) 2001-02-02 2002-01-26 抗血栓性化合物、その製法及び医薬組成物としての使用
MXPA03006648A MXPA03006648A (es) 2001-02-02 2002-01-26 Compuestos antitombroticos, su preparacion y su utilizacion como medicamentos.

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE10104597A DE10104597A1 (de) 2001-02-02 2001-02-02 Antithrombotische Verbindungen, deren Herstellung und deren Verwendung als Arzneimittel
DE10104597.2 2001-02-02
DE10135435.0 2001-07-26
DE10135435 2001-07-26

Publications (2)

Publication Number Publication Date
WO2002062778A2 WO2002062778A2 (de) 2002-08-15
WO2002062778A3 true WO2002062778A3 (de) 2003-12-11

Family

ID=26008392

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/000823 Ceased WO2002062778A2 (de) 2001-02-02 2002-01-26 Antithrombotische verbindungen, deren herstellung und deren verwendung als arzneimittel

Country Status (5)

Country Link
EP (1) EP1390357A2 (de)
JP (1) JP2004522759A (de)
CA (1) CA2435492A1 (de)
MX (1) MXPA03006648A (de)
WO (1) WO2002062778A2 (de)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030181488A1 (en) 2002-03-07 2003-09-25 Boehringer Ingelheim Pharma Gmbh & Co. Kg Administration form for the oral application of 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester and the salts thereof
DE10234058A1 (de) * 2002-07-26 2004-02-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Benzoesäureamide, deren Herstellung und deren Verwendung als Arzneimittel
PL374971A1 (en) * 2002-08-09 2005-11-14 Transtech Pharma, Inc. Aryl and heteroaryl compounds and methods to modulate coagulation
US7247654B2 (en) 2003-06-04 2007-07-24 Bristol-Myers Squibb Company 3,4-disubstituted benzamidines and benzylamines, and analogues thereof, useful as serine protease inhibitors
US7570259B2 (en) 2004-06-01 2009-08-04 Intel Corporation System to manage display power consumption
WO2006027135A1 (en) * 2004-09-06 2006-03-16 F. Hoffmann-La Roche Ag 4-aminomethyl benzamidine derivatives and their use as factor viiia inhibitors
ATE405553T1 (de) 2004-12-08 2008-09-15 Bristol Myers Squibb Co Heterocyclische verbindungen als inhibitoren von faktor viia
BRPI0710487A2 (pt) 2006-04-12 2012-06-05 Merck & Co Inc composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitácel do mesmo e, método para tratar ou controlar a epilepsia e a dor e para o tratamento ou prevenção de um distúrbio do sono em um paciente.
BRPI0818244A2 (pt) 2007-10-24 2015-06-16 Merck Sharp & Dohme Composto, composição farmacêutica, uso de um composto, e, método para tratamento de um distúrbio ou doença
BR112016030690B1 (pt) 2014-06-27 2023-11-14 Nogra Pharma Limited Compostos moduladores do receptor de arila, composição farmacêutica compreendendo os mesmos e usos terapêuticos dos ditos compostos

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2007663A (en) * 1977-11-07 1979-05-23 Dresden Arzneimittel Sulphonylated omega - amidinophenyl- alpha -aminocarhoxylic acid amides
EP0654465A1 (de) * 1993-11-15 1995-05-24 Ciba-Geigy Ag Polyaminopolyamide
WO1996040100A1 (en) * 1995-06-07 1996-12-19 3-Dimensional Pharmaceuticals, Inc. ARYLSULFONYLAMINOBENZENE DERIVATIVES AND THE USE THEREOF AS FACTOR Xa INHIBITORS
WO2000056707A1 (en) * 1999-03-24 2000-09-28 Sepracor, Inc. Diaryl thioethers, compositions and uses thereof
WO2001010823A1 (de) * 1999-08-07 2001-02-15 Boehringer Ingelheim Pharma Kg Carbonsäureamide, deren herstellung und deren verwendung als arzneimittel
WO2002004403A1 (de) * 2000-07-08 2002-01-17 Boehringer Ingelheim Pharma Kg Biphenylcarbonsäureamide, ihre herstellung und ihre verwendung als arzneimittel

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2007663A (en) * 1977-11-07 1979-05-23 Dresden Arzneimittel Sulphonylated omega - amidinophenyl- alpha -aminocarhoxylic acid amides
EP0654465A1 (de) * 1993-11-15 1995-05-24 Ciba-Geigy Ag Polyaminopolyamide
WO1996040100A1 (en) * 1995-06-07 1996-12-19 3-Dimensional Pharmaceuticals, Inc. ARYLSULFONYLAMINOBENZENE DERIVATIVES AND THE USE THEREOF AS FACTOR Xa INHIBITORS
WO2000056707A1 (en) * 1999-03-24 2000-09-28 Sepracor, Inc. Diaryl thioethers, compositions and uses thereof
WO2001010823A1 (de) * 1999-08-07 2001-02-15 Boehringer Ingelheim Pharma Kg Carbonsäureamide, deren herstellung und deren verwendung als arzneimittel
WO2002004403A1 (de) * 2000-07-08 2002-01-17 Boehringer Ingelheim Pharma Kg Biphenylcarbonsäureamide, ihre herstellung und ihre verwendung als arzneimittel

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
ARCH. PHARM., vol. 315, no. 12, 1982, pages 1003 - 1007 *
BIOORG. MED. CHEM. LETT., vol. 10, no. 24, 2000, pages 2741 - 2744 *
CHEMICAL ABSTRACTS, vol. 98, no. 7, 1983, Columbus, Ohio, US; abstract no. 53340r, VALENTI, PIERO ET AL.: "Cyclovinylogs of procainamide" page 620; column 1; XP002232678 *
DATABASE CROSSFIRE BEILSTEIN BEILSTEIN INSTITUT ZUR FOERDERUNG DER CHEMISCHEN WISSENSCHAFTEN, FRANKFURT AM MAIN, DE; XP002232679 *
LABES D ET AL: "Free-Wilson-Analyse der Hemmwirkung von 4-substituierten Benzamidinen gegenueber Thrombin, Plasmin und Trypsin", PHARMAZIE, VEB VERLAG VOLK UND GESUNDHEIT. BERLIN, DD, vol. 34, no. 9, 1979, pages 554 - 555, XP002152595, ISSN: 0031-7144 *
TAMIZ A P ET AL: "A convenient procedure for the synthesis of nonsymmetrical bivalent selective serotonin reuptake inhibitors using polymer-supported reagents", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 10, no. 24, 18 December 2000 (2000-12-18), pages 2741 - 2743, XP004225340, ISSN: 0960-894X *

Also Published As

Publication number Publication date
CA2435492A1 (en) 2002-08-15
EP1390357A2 (de) 2004-02-25
JP2004522759A (ja) 2004-07-29
WO2002062778A2 (de) 2002-08-15
MXPA03006648A (es) 2003-10-15

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